ES2191484T3 - HETEROCICLICAL COMPOUNDS AS INHIBITORS OF ROTAMASA ENZYMES. - Google Patents

HETEROCICLICAL COMPOUNDS AS INHIBITORS OF ROTAMASA ENZYMES.

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Publication number
ES2191484T3
ES2191484T3 ES99963123T ES99963123T ES2191484T3 ES 2191484 T3 ES2191484 T3 ES 2191484T3 ES 99963123 T ES99963123 T ES 99963123T ES 99963123 T ES99963123 T ES 99963123T ES 2191484 T3 ES2191484 T3 ES 2191484T3
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Spain
Prior art keywords
alkyl
aryl
independently selected
halogen
cycloalkyl
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES99963123T
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Spanish (es)
Inventor
Mark Ian Kemp
Michael John Palmer
Mark Allen Sanner
Martin James Wythes
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Pfizer Inc
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Pfizer Inc
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Publication date
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Publication of ES2191484T3 publication Critical patent/ES2191484T3/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un compuesto de fórmula (I): **(Fórmula)** o una sal farmacéuticamente aceptable del mismo, en el que A es un alquileno C3 - C5 no ramificado opcionalmente sustituido con un alquilo C1 - C6; X es O, S, NH o N(alquilo C1 - C6); Y es O, S, NH o N(alquilo C1 - C6); R es un grupo heterocíclico de anillo no aromático de 4 a 6 eslabones unido por un átomo de carbono, que contiene un heteroátomo de nitrógeno, estando dicho grupo opcionalmente sustituído con 1, 2, ó 3 sustituyente(s) cada uno de ellos independientemente seleccionado de alquilo C1 - C6, alquenilo C2 - C6, cicloalquilo C3 - C7, arilo, het, - CO2 (alquilo C1 - C6), - CO (het), - CONR5R6 y - CO (arilo), estando dicho alquilo y alquenilo opcionalmente sustituidos por 1 ó 2 sustituyente(s) cada uno de ellos seleccionados independientemente de cicloalquilo C3 - C7, arilo, het, - O (arilo), - O (alquileno C1 - C2)arilo, - CO (het), - CONR5R6 y - CO (arilo); R1, R2, R3 y R4 se seleccionan independientemente de H, halógeno, alquilo C1 - C6,cicloalquilo C3 - C7, haloalquilo C1 - C6), alcoxi C1 - C6, - CONR5R6, cicloalcoxi C3 - C7, cicloalquilo C3 - C7 - alquileno (C2 - C4), cicloalquilo (C3 - C7)alcoxi (C2 - C4) y - CO2(alquilo C1 - C6); R5 y R6 son, bien cada uno de ellos independientemente seleccionados entre H y alquilo C1 - C6, o bien, cuando se consideran juntos, representan un alquileno C3 - C5 no ramificado; ¿arilo¿ significa fenilo, opcionalmente sustituido con 1, 2 ó 3 sustituyente(s) cada uno de ellos independientemente seleccionado entre alquilo C1 - C6, alcoxi C1 - C6, halógeno, CONR5R6, halógeno(alquilo C1 - C6) y - NR5R6; y ¿het¿ significa un grupo heterocíclico de anillo monocíclico de 5 ó 6 eslabones, o de anillo bicíclico de 8, 9 ó 10 eslabones, que contiente de 1 a 3 heteroátomos cada uno de ellos independientemente seleccionado entre N, O y S, dicho grupo puede estar opcionalmente sustituido con 1, 2 ó 3 sustituyente(s) cada uno de ellos seleccionado independientemente entre alquilo C1 - C6, alcoxi C1 - C6,halógeno, halógeno(alquilo C1 - C6), fenilo y - NR5R6.A compound of formula (I): ** (Formula) ** or a pharmaceutically acceptable salt thereof, wherein A is an unbranched C3-C5 alkylene optionally substituted with a C1-C6 alkyl; X is O, S, NH or N (C1-C6 alkyl); Y is O, S, NH or N (C1-C6 alkyl); R is a non-aromatic ring heterocyclic group of 4 to 6 links linked by a carbon atom, which contains a nitrogen heteroatom, said group being optionally substituted with 1, 2, or 3 substituents (s) each independently selected of C1-C6 alkyl, C2-C6 alkenyl, C3-C7 cycloalkyl, aryl, het, -C02 (C1-C6 alkyl), -CO (het),-CONR5R6 and -CO (aryl), said alkyl and alkenyl being optionally substituted by 1 or 2 substituent (s) each independently selected from C3-C7 cycloalkyl, aryl, het, - O (aryl), - O (C1-C2 alkylene) aryl, - CO (het), - CONR5R6 and - CO (aryl); R1, R2, R3 and R4 are independently selected from H, halogen, C1-C6 alkyl, C3-C7 cycloalkyl, C1-C6 haloalkyl), C1-C6 alkoxy, - CONR5R6, C3-C7 cycloalkoxy, C3-C7-alkylene cycloalkyl (C2-C4), cycloalkyl (C3-C7) alkoxy (C2-C4) and-CO2 (C1-C6 alkyl); R5 and R6 are either independently selected from H and C1-C6 alkyl, or, when considered together, represent an unbranched C3-C5 alkylene; "Aryl" means phenyl, optionally substituted with 1, 2 or 3 substituent (s) each independently selected from C1-C6 alkyl, C1-C6 alkoxy, halogen, CONR5R6, halogen (C1-C6 alkyl) and-NR5R6; and does het mean a heterocyclic group of a monocyclic ring of 5 or 6 links, or of a bicyclic ring of 8, 9 or 10 links, containing 1 to 3 heteroatoms each independently selected from N, O and S, said group may be optionally substituted with 1, 2 or 3 substituent (s) each independently selected from C1-C6 alkyl, C1-C6 alkoxy, halogen, halogen (C1-C6 alkyl), phenyl and -NR5R6.

ES99963123T 1998-07-21 1999-06-28 HETEROCICLICAL COMPOUNDS AS INHIBITORS OF ROTAMASA ENZYMES. Expired - Lifetime ES2191484T3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9815880.1A GB9815880D0 (en) 1998-07-21 1998-07-21 Heterocycles

Publications (1)

Publication Number Publication Date
ES2191484T3 true ES2191484T3 (en) 2003-09-01

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ES99963123T Expired - Lifetime ES2191484T3 (en) 1998-07-21 1999-06-28 HETEROCICLICAL COMPOUNDS AS INHIBITORS OF ROTAMASA ENZYMES.

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US (2) US6372736B1 (en)
EP (1) EP1100797B1 (en)
JP (2) JP3795329B2 (en)
KR (2) KR100450008B1 (en)
CN (3) CN1511837A (en)
AP (1) AP2001002046A0 (en)
AR (1) AR019427A1 (en)
AT (1) ATE233261T1 (en)
AU (1) AU765925B2 (en)
BG (1) BG105254A (en)
BR (1) BR9912330A (en)
CA (1) CA2338214C (en)
CO (1) CO5080782A1 (en)
CR (1) CR6073A (en)
DE (1) DE69905582T2 (en)
DK (1) DK1100797T3 (en)
DZ (1) DZ2851A1 (en)
EA (1) EA003513B1 (en)
EE (1) EE200100044A (en)
ES (1) ES2191484T3 (en)
GB (1) GB9815880D0 (en)
GE (1) GEP20033028B (en)
GT (1) GT199900115A (en)
HK (1) HK1039779A1 (en)
HN (1) HN1999000106A (en)
HR (1) HRP20010052A2 (en)
HU (1) HUP0103413A3 (en)
ID (1) ID26991A (en)
IL (1) IL140244A0 (en)
IS (1) IS5790A (en)
MA (1) MA24936A1 (en)
MY (1) MY118222A (en)
NO (1) NO20010322L (en)
NZ (2) NZ508838A (en)
OA (1) OA11585A (en)
PA (1) PA8478501A1 (en)
PE (1) PE20001037A1 (en)
PL (1) PL345734A1 (en)
SI (1) SI1100797T1 (en)
SK (1) SK772001A3 (en)
SV (1) SV1999000102A (en)
TN (1) TNSN99147A1 (en)
TR (1) TR200100135T2 (en)
TW (1) TWI229672B (en)
WO (1) WO2000005232A1 (en)

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CN1511837A (en) 2004-07-14
EP1100797A1 (en) 2001-05-23
CA2338214A1 (en) 2000-02-03
DE69905582T2 (en) 2003-09-04
AU765925B2 (en) 2003-10-02
CN1611499A (en) 2005-05-04
MY118222A (en) 2004-09-30
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